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首页> 外文期刊>European journal of pharmaceutical sciences >Characterization and evaluation of nanostructured lipid carrier as a vehicle for oral delivery of etoposide.
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Characterization and evaluation of nanostructured lipid carrier as a vehicle for oral delivery of etoposide.

机译：表征和评价纳米结构脂质载体作为依托泊苷口服给药的载体。

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Nanostructured lipid carriers (NLCs) are a new generation of lipid nanoparticles, which have showed some advantages over traditional lipid nanoparticles, such as improved drug incorporation and release properties. The purpose of this study is to develop an optimized nanostructured lipid carrier formulation for etoposide (VP16), and to estimate the potential of NLCs as oral delivery system. VP16-NLCs were prepared by an emulsification and low-temperature solidification method. The average drug entrapment efficiency, particle size and zeta potential of VP16-NLCs, VP16-PEG40-St-modified NLCs (VP16-PEG40-NLCs) and VP16-DSPE-PE- modified NLCs (VP16-DSPE-NLCs) were 57.9-89.7%, 125.9-91.2 nm and -28.49 to -15.34 mV, respectively. The absorption of VP16-NLCs in the intestine was performed by the diffusion chamber. It was found that VP16-DSPE-NLCs with a smaller particle size made the drug transport easy from mucosal to serosal side. A pharmacokinetic study was conducted in rats. After oral administration of VP16 at a dose of 180 mg/kg in the form of either VP16-NLCs or suspension, the relative bioavailability of VP16-NLCs, VP16-PEG40-NLCs and VP16-DSPE-NLCs were enhanced about 1.8-, 3.0- and 3.5-fold, respectively, compared with VP16 suspension. Furthermore, VP16-DSPE-NLCs displayed the highest cytotoxicity against human epithelial-like lung carcinoma cells. The NLCs formulation remarkably improved the oral bioavailability of VP16 and demonstrated a promising perspective for oral delivery of VP16.
机译：纳米结构脂质载体（NLC）是新一代脂质纳米颗粒，与传统脂质纳米颗粒相比，它们具有一些优势，例如改善了药物的结合和释放特性。这项研究的目的是开发一种针对依托泊苷（VP16）的优化的纳米结构脂质载体制剂，并评估NLC作为口服给药系统的潜力。 VP16-NLC通过乳化和低温固化方法制备。 VP16-NLC，VP16-PEG40-St修饰的NLC（VP16-PEG40-NLC）和VP16-DSPE-PE修饰的NLC（VP16-DSPE-NLC）的平均药物截留效率，粒径和Zeta电位为57.9-分别为89.7％，125.9-91.2 nm和-28.49至-15.34 mV。 VP16-NLC在肠中的吸收是通过扩散室进行的。发现具有较小粒径的VP16-DSPE-NLC使药物易于从粘膜侧转移到浆膜侧。在大鼠中进行了药代动力学研究。以VP16-NLC或混悬液形式口服VP16剂量为180 mg / kg后，VP16-NLC，VP16-PEG40-NLC和VP16-DSPE-NLC的相对生物利用度提高了约1.8-，3.0与VP16悬浮液相比，分别是-和3.5倍。此外，VP16-DSPE-NLC对人上皮样肺癌细胞显示出最高的细胞毒性。 NLCs配方显着提高了VP16的口服生物利用度，并证明了VP16口服给药的前景广阔。

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